476314-25-7Relevant academic research and scientific papers
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-α) production
Laughlin, Steven K.,Clark, Michael P.,Djung, Jane F.,Golebiowski, Adam,Brugel, Todd A.,Sabat, Mark,Bookland, Roger G.,Laufersweiler, Matthew J.,VanRens, John C.,Townes, Jennifer A.,De, Biswanath,Hsieh, Lily C.,Xu, Susan C.,Walter, Richard L.,Mekel, Marlene J.,Janusz, Michael J.
, p. 2399 - 2403 (2005)
4-Aryl-3-pyridyl and 4-aryl-3-pyrimidinyl based tumor necrosis factor-alpha (TNF-α) inhibitors, which contain a novel isoxazolone five-membered heterocyclic core are described. Many showed sub-micromolar activity against lipopolysaccharide-induced TNF-α production.
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors
Townes, Jennifer A.,Golebiowski, Adam,Clark, Michael P.,Laufersweiler, Matthew J.,Brugel, Todd A.,Sabat, Mark,Bookland, Roger G.,Laughlin, Steve K.,VanRens, John C.,De, Biswanath,Hsieh, Lily C.,Xu, Susan C.,Janusz, Michael J.,Walter, Richard L.
, p. 4945 - 4948 (2007/10/03)
4-Aryl-5-pyrimidyl-based cytokine synthesis inhibitors of TNF-α production, which contain a novel bicyclic pyrazole heterocyclic core, are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-α production in a THP-1 cell-based assay and against human p38α MAP kinase in an isolated enzyme assay. The X-ray crystal structure of a bicyclic pyrazole inhibitor co-crystallized with mutated p38 (mp38) is presented. 4-Aryl-5-pyrimidyl-based cytokine synthesis inhibitors of TNF-α production, which contain a novel bicyclic pyrazole heterocyclic core, are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-α production in a THP-1 cell-based assay and against human p38α MAP kinase in an isolated enzyme assay. The X-ray crystal structure of a bicyclic pyrazole inhibitor co-crystallized with mutated p38 (mp38) is presented.
Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity
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, (2008/06/13)
Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis,
